M. Ishihara et al., IMPORTANCE OF 2-O-SULFATE GROUPS OF URONATE RESIDUES IN HEPARIN FOR ACTIVATION OF FGF-1 AND FGF-2, Journal of Biochemistry, 121(2), 1997, pp. 345-349
Complete drying of heparin with various concentrations of NaOH by lyop
hilization caused specific 2-O-desulfation to various degrees without
detectable depolymerization or other chemical changes. In order to ass
ess the importance of 2-O-sulfate groups in uronate residues to promot
e FGF-1 and FGF-2 activities, various 2-O-desulfated (2-O-DS-) heparin
s were quantitatively examined for their effects on FGF-1- and FGF-2-i
nduced proliferation of BALB/c3T3 clone A31 (A31) cells and the chlora
te-treated cells. Twenty-seven percent or less loss of the 2-O-sulfate
groups had no effect on the ability to activate both FGF-1 and FGF-2,
while 44% loss resulted in a significant loss of the ability. Complet
e loss of the ability was observed in 2-O-DS-heparins with 75% or more
2-O-desulfation. These results suggest that a high content of 2-O-sul
fate groups in uronate residues of heparin is required for activation
of both FGF-1 and FGF-2.